KJ Pyr 9 is a small-molecule inhibitor of MYC. The Kd of KJ Pyr 9 for MYC in vitro is 6.5±1.0 nM, as determined by backscattering interferometry.
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产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SBI-0206965 |
+++
ULK1, IC50: 108 nM ULK2, IC50: 711 nM |
97% | |||||||||||||||||
Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
MRT68921 hydrochloride |
++++
ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM |
99%+ | |||||||||||||||||
ROC-325 | ✔ | 99%+ | |||||||||||||||||
Autophinib |
+++
Autophagy, IC50: 40 nM |
97% | |||||||||||||||||
Lys05 | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | KJ Pyr 9 (KJ-Pyr-9) acts by disrupting the MYC-MAX complex formation within cells, as observed in protein fragment complementation assays[1]. KJ Pyr 9 specifically targets and inhibits MYC-induced oncogenic transformation in cell cultures, showing minimal or negligible impact on the oncogenic functions of various unrelated oncoproteins[1]. KJ Pyr 9 notably affects the proliferation of cells overexpressing MYC, both human and avian, and distinctively reduces the transcriptional signature driven by MYC[1]. KJ Pyr 9 efficacy has been tested against three cell lines known for their dependence on enhanced MYC activity: NCI-H460, MDA-MB-231, and SUM-159PT, successfully inhibiting their proliferation with IC50 values ranging between 5 and 10 μM[1]. Burkitt lymphoma cell lines, characterized by constitutively high c-MYC expression, show even greater sensitivity to KJ Pyr 9, with IC50 values between 1 and 2.5 μM[1]. |
体内研究 | Additionally, KJ Pyr 9 administered intraperitoneally at 10 mg/kg daily for 31 days has been found capable of arresting tumor growth[1]. |
体外研究 | KJ Pyr 9 (KJ-Pyr-9) acts by disrupting the MYC-MAX complex formation within cells, as observed in protein fragment complementation assays[1]. KJ Pyr 9 specifically targets and inhibits MYC-induced oncogenic transformation in cell cultures, showing minimal or negligible impact on the oncogenic functions of various unrelated oncoproteins[1]. KJ Pyr 9 notably affects the proliferation of cells overexpressing MYC, both human and avian, and distinctively reduces the transcriptional signature driven by MYC[1]. KJ Pyr 9 efficacy has been tested against three cell lines known for their dependence on enhanced MYC activity: NCI-H460, MDA-MB-231, and SUM-159PT, successfully inhibiting their proliferation with IC50 values ranging between 5 and 10 μM[1]. Burkitt lymphoma cell lines, characterized by constitutively high c-MYC expression, show even greater sensitivity to KJ Pyr 9, with IC50 values between 1 and 2.5 μM[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.59mL 0.52mL 0.26mL |
12.97mL 2.59mL 1.30mL |
25.95mL 5.19mL 2.59mL |
CAS号 | 581073-80-5 |
分子式 | C22H15N3O4 |
分子量 | 385.372 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Room Temperature |
溶解度 |
DMSO: 120 mg/mL(311.39 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |